Go toArchive
Browse byFacets
Bookbag ( 0 )
'Solid Phase Peptide Synthesis' in keywords Facet   Publication Year 1995  [X]
Facet   section ZfN Section B:Volume 050  [X]
Results  1 Item
Sorted by   
Publication Year
1995[X]
1Author    Anna Janecka3, StevenK. Oerberb, Tomasz Janecki3, Cyril Bowersc, Karl Folkers3Requires cookie*
 Title    N5-PyrazinylcarbonyIornithine, an Effective Substituent for Position 5 of Antagonists of LHRH  
 Abstract    Com puter modeling was used to find an effective substituent for position 5 in antagonists of the luteinizing hormone-releasing hormone (LHRH). In particular, it was desired to replace ds-3-(4-pyrazinylcarbonylaminocyclohexyl)alanine in position 5 because this sub­ stituent is laborious to synthesize. Calculations revealed that N5-pyrazinylcarbonylornithine (PzOrn) should be a suitable substitute for cPzACAla, with N6-pyrazinylcarbonyllysine (PzLys) being a second choice. Twelve analogs were synthesized in four series with DNal or DQal in position 1 and ILys or Arg in position 8. Biological assays validated the calculations and show that antagonists with PzOrn are more potent in antiovulatory assay than antag­ onists with PzLys. The antagonists with PzOrn were comparable in AOA with antagonists with cPzACAla. What is also im portant, antagonists with PzOrn released significantly less histamine than those with cPzACAla. 
  Reference    Z. Naturforsch. 50b, 147—150 (1995); received April 27 1994 
  Published    1995 
  Keywords    LH RH Antagonists, Com puter Modeling, Antiovulatory Activity, Histamine Release, Solid Phase Peptide Synthesis 
  Similar Items    Find
 DEBUG INFO      
 TEI-XML for    default:Reihe_B/50/ZNB-1995-50b-0147.pdf 
 Identifier    ZNB-1995-50b-0147 
 Volume    50